生物活性：
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.

体内活性：
Tazemetostat (EPZ-6438；250 或 500 mg/kg，每天两次，持续 21-28 天) 几乎可以消除快速生长的 G401 肿瘤。

体外活性：
Tazemetostat (EPZ-6438) 抑制多种野生型和突变型淋巴瘤细胞系增殖，IC50 为 0.49 Nm-7.6 Μm。